桧木醇衍生物的合成及抑菌活性  

Synthesis and antifungal activity of hinokitiol derivatives

作　　者：桂阔 叶久辉 李璇 周海玉 李婕宁 冯俊涛 雷鹏 高艳清 马志卿 GUI Kuo;YE Jiuhui;LI Xuan;ZHOU Haiyu;LI Jiening;FENG Juntao;LEI Peng;GAO Yanqing;MA Zhiqing(College of Plant Protection,Northwest A&F University,Shaanxi Research Center of Biopesticide Engineering&Technology,Yangling 712100,Shaanxi Province,China)

机构地区：[1]西北农林科技大学植物保护学院,陕西省生物农药工程技术研究中心,陕西杨凌712100

出　　处：《农药学学报》2023年第1期73-80,共8页Chinese Journal of Pesticide Science

基　　金：广西林产化学与工程重点实验开放课题(GXFG 2009);陕西省专项经费(F2020221004);国家级大学生创新创业训练计划项目(202210712071)。

摘　　要：桧木醇是具有?酚酮骨架的单萜类天然化合物,设计并合成了17个新型桧木醇衍生物,其结构经核磁共振波谱及高分辨质谱分析确证。抑菌活性测定结果表明,目标化合物在50μg/mL下对水稻纹枯病菌Rhizoctonia solani、番茄灰霉病菌Botrytis cinerea、油菜菌核病菌Sclerotinia sclerotiorum、苹果树腐烂病菌Valsa mali和黄瓜炭疽病菌Colletotrichum orbiculare均表现出较好的抑菌活性,其中化合物3a对水稻纹枯病菌、3j对番茄灰霉病菌、3m对油菜菌核病菌的EC_(50)值分别为1.84、2.47和1.05μg/mL,表现出比桧木醇(2.00、11.3和5.40μg/mL)更优的活性。Seventeen novel derivatives of hinokitiol,a monoterpene with a troponoide skeleton,were designed and synthesized.Their structures were confirmed by NMR and HRMS.The in vitro bioassay results showed that the target compounds displayed satisfactory antifungal activities against Rhizoctonia solani,Botrytis cinerea,Sclerotinia sclerotiorum,Valsa mali and Colletotrichum orbiculare at50μg/mL.Notably,compound 3a showed favorable activity against R.solani(EC_(50)=1.84μg/mL),3j exhibited satisfied activity against B.cinerea(EC_(50)=2.47μg/mL),and 3m exerted excellent activity against S.sclerotiorum(EC_(50)=1.05μg/mL),which are better than hinokitiol(2.00,11.3 and5.40μg/mL).

关 键 词：桧木醇 水稻纹枯病菌 番茄灰霉病菌 油菜菌核病菌 抑菌活性 

分 类 号：TQ450.1[化学工程—农药化工] TQ455